Repotrectinib (TPX-0005)

Catalog No.S8583

For research use only.

Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).

Repotrectinib (TPX-0005) Chemical Structure

CAS No. 1802220-02-5

Selleck's Repotrectinib (TPX-0005) has been cited by 6 Publications

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Biological Activity

Description Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
Targets
ROS1 [2] Trk receptor [2] WT ALK [1]
(Cell-free assay)
ALK(L1196M) [1]
(Cell-free assay)
ALK(G1202R) [1]
(Cell-free assay)
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1.01 nM 1.08 nM 1.26 nM
In vitro

TPX-0005 is an orally available and potent ATP-competitive inhibitor against ALK, ROS1, TRKA, TRKB and TRKC recombinant kinases and their corresponding clinical resistant mutants. TPX-0005 demonstrates potent anti-proliferative activity in the range of sub-nanomolar to low nanomolar in a number of human cancer cell lines and engineered stable cell lines expressing the targeted oncogenes or their solvent front mutants, accompanied by inhibition of target phosphorylation and concomitant inactivation of downstream effectors such as ERK, AKT and STAT3[2]. TPX-0005 inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib. TPX-0005 is able to not only inhibit the wild-type and a broad spectrum of mutant ALKs, but also overcome primary resistance and suppress metastatic features by inhibiting SRC[1].

Assay
Methods Test Index PMID
Western blot pEGFR / pERK / pAKT / pSTAT3 / pPaxillin / Pyap1 / cleaved caspase-3 29433983
Immunofluorescence pSTAT3(Y705) / STAT3 29433983
In vivo In patient derived xenograft tumor models, TPX-0005 treatment results in significant regression of tumors harboring the oncogenic ALK, ROS1 and TRKC fusions. Moreover, in a series of mouse xenograft tumor models, TPX-0005 exhibits marked anti-tumor activity not only in tumors harboring the wildtype oncogenic targets but also in tumors harboring the oncogenes with the solvent front mutations via inhibition of the target phosphorylation[2].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 355.37
Formula

C18H18FN5O2

CAS No. 1802220-02-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CNC(=O)C2=C3N=C(C=CN3N=C2)NC(C4=C(O1)C=CC(=C4)F)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03093116 Recruiting Drug: Oral repotrectinib (TPX-0005) Locally Advanced Solid Tumors|Metastatic Solid Tumors Turning Point Therapeutics Inc. February 27 2017 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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